title: Design, synthesis and biological activity of thiazolidine-4-carboxylic acid derivatives as novel influenza neuraminidase inhibitors.
abstract: A series of thiazolidine-4-carboxylic acid derivatives were synthesized and evaluated for their ability to inhibit neuraminidase (NA) of influenza A virus. All the compounds were synthesized in good yields starting from commercially available l-cysteine hydrochloride using a suitable synthetic strategy. These compounds showed moderate inhibitory activity against influenza A neuraminidase. The most potent compound of this series is compound 4f (IC(50)=0.14 μM), which is about sevenfold less potent than oseltamivir and could be used to design novel influenza NA inhibitors that exhibit increased activity based on thiazolidine ring.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44 West Wenhua Road, Jinan, Shandong 250012, China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Liu
authors.forename: Fanbo
authors.initials: F
authors.lastname: Jing
authors.forename: Yingying
authors.initials: Y
authors.lastname: Xu
authors.forename: Yuanchao
authors.initials: Y
authors.lastname: Xie
authors.forename: Fangyuan
authors.initials: F
authors.lastname: Shi
authors.forename: Hao
authors.initials: H
authors.lastname: Fang
authors.forename: Minyong
authors.initials: M
authors.lastname: Li
authors.forename: Wenfang
authors.initials: W
authors.lastname: Xu
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015195:Drug Design; D053122:Influenza A Virus, H3N2 Subtype / Q000201:enzymology*; D008958:Models, Molecular; D009439:Neuraminidase / Q000037:antagonists & inhibitors* / Q000737:chemistry; D053139:Oseltamivir / Q000737:chemistry / Q000494:pharmacology; D053778:Thiazolidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000998:Antiviral Agents; D053778:Thiazolidines; D053139:Oseltamivir; C003438:thiazolidine-4-carboxylic acid; D009439:Neuraminidase